Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemESOS1-IN-21Cat.No.:HY-175326CASNo.:2767633-04-3分子式:C??H??F?N?O?分子量:493.52作用靶點:SOS1作用通路:MAPK/ERKPathway儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性SOS1-IN-21是一種口服有效的sonofSevenless1(SOS1)抑制劑，其IC50值為15nM。SOS1是一種鳥嘌呤核苷酸交換因子(GEF)，通過促進(jìn)GDP到GTP的轉(zhuǎn)換來激活KRAS。SOS1-IN-21具有強(qiáng)大的抗增殖活性，對NCI-H358細(xì)胞的IC50值為16nM，對MiaPaca-2細(xì)胞為17nM。SOS1-IN-21在MiaPaca-2腫瘤移植模型中表現(xiàn)出顯著的抗腫瘤活性。SOS1-IN-21可用于研究KRAS突變腫瘤，如胰腺癌[1]。體外研究SOS1-IN-21(Compound21)(0-3000nM)significantlyenhancesgrowthsuppressioninMiaPaCa-2cellsincombinationoftheKRASG12CinhibitorAMG510(HY-114277)[1].體內(nèi)研究SOS1-IN-21(Compound21)(12-50mg/kg,p.o.,twicedaily,for23days)significantlyinhibitstumorgrowthandtheeffectisenhancedwithAMG510inMiaPaCa-2xenograftmodel[1].AnimalModel:MiaPaCa-2tumorcellsinducedxenograftmodelestablishedinBALB/cnudemice[1]Dosage:12mg/kg(Day0-9)and50mg/kg(Day9-23)Administration:Oraladministration(p.o.),for23daysResult:Showedatumorinhibitionrateof38%attheendofthe23-day.ResultedinasynergisticeffectontumorcellgrowthinhibitionwithAMG510.REFERENCES[1].LvY,etal.APotentSOS1PROTACDegraderwithSynergisticEfficacyinCombinationwithKRASG12CInhibitor.JMedChem.20241/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEFeb22;67(4):2487-2511.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792/p>